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Naftifine hydrochloride

Naftifine hydrochloride

产品编号 T1543   CAS 65473-14-5
别名: Naftifungin, 盐酸萘替芬, Naftifine HCl, Naftin, Exoderil

Naftifine hydrochloride (Naftifine HCl) 是一种抗生素。它具有抗真菌活性,对皮肤真菌、曲霉、Sporothrix schenckii、假丝酵母属的酵母有抑制作用。

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Naftifine hydrochloride Chemical Structure
Naftifine hydrochloride, CAS 65473-14-5
规格 价格/CNY 货期 数量
50 mg ¥ 247 现货
100 mg ¥ 348 现货
500 mg ¥ 838 现货
1 g ¥ 1,390 现货
其他形式的 Naftifine hydrochloride:
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千万补贴 助力科研
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产品目录号及名称: Naftifine hydrochloride (T1543)
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纯度: 99.84%
纯度: 99.76%
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生物活性
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参考文献
产品描述 Naftifine Hydrochloride is the hydrochloride salt form of naftifine, an allylamine derivate with synthetic broad-spectrum antifungal activity. Although the exact mechanism through which naftifine hydrochloride exerts its effect is unknown, it appears to selectively inhibit the enzyme squalene 2, 3-epoxidase, thereby inhibiting the biosynthesis of sterol. This results in a decreased amount of sterols, especially ergosterol which is the primary fungal membrane sterol, and a corresponding accumulation of squalene in fungal cells. Naftifine hydrochloride (Naftifine HCl) can be fungicidal as well as fungistatic to yeasts depending on the concentration and the organisms involved.
体外活性 Naftifine exhibits an interesting in vitro spectrum of activity against dermatophytes (38 strains; minimal inhibitory concentration (MIC) range 0.1 to 0.2 mg/mL), aspergilli (6 strains; MIC range, 0.8 to 12.5 mg/mL), Sporothrix schenckii (2 strains; MICs, 0.8 and 1.5 mg/mL), and yeasts of the genus Candida (77 strains; MIC range, 1.5 to greater than 100 mg/mL). [1] The MIC of naftifine for C. albicans Δ63 is 100 mg/L in Sabouraud medium (initial pH 6.5). Naftifine (50 mg/L) gives greater than 99% inhibition of sterol biosynthesis both in whole cells and in cell extracts of C. albicans. The primary action of naftifine appears to be the blocking of fungal squalene epoxidation. [2]
体内活性 Naftifine HCl 2% cream results in clinical cure rate and clinical success rate of 33% and 84% after treatment for 4 weeks, and week 2 efficacy response rates in Naftifine HCl 2% subjects are all lower than at week 4 but are significantly higher than week 2 vehicle-treated counterparts. [3] Naftifine causes interruption of fungal ergosterol synthesis and accumulation of squalene in fungal organisms. Naftifine also has demonstrated anti-inflammatory properties such as a reduction in superoxide production and a reduction in polymorphonuclear leukocyte chemotaxis/endothelial adhesion. Naftifine has shown good efficacy and safety for a variety of conditions and is a useful treatment that provides both antifungal action and relief of inflammatory signs and symptoms. Few adverse events have been noted with naftifine use, the most frequent being mild and transient burning, stinging, or itching in the application area. [4]
别名 Naftifungin, 盐酸萘替芬, Naftifine HCl, Naftin, Exoderil
分子量 323.86
分子式 C21H22ClN
CAS No. 65473-14-5

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 8 mg/mL (24.7 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
Ethanol 1 mM 3.0878 mL 15.4388 mL 30.8775 mL 77.1938 mL
5 mM 0.6176 mL 3.0878 mL 6.1755 mL 15.4388 mL
10 mM 0.3088 mL 1.5439 mL 3.0878 mL 7.7194 mL
20 mM 0.1544 mL 0.7719 mL 1.5439 mL 3.8597 mL

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TargetMol Library Books参考文献

1. Georgopoulos A, et al. Antimicrob Agents Chemother, 1981, 19(3), 386-389. 2. Ryder NS, et al. Antimicrob Agents Chemother, 1984, 25(4), 483-487. 3. Parish LC, et al. J Drugs Dermatol, 2011, 10(10), 1142-1147. 4. Gupta AK, et al. J Cutan Med Surg, 2008, 12(2), 51-58.
Triparanol SANT-1 Sonidegib Jervine SMANT hydrochloride JK184 SAG dihydrochloride Tolnaftate

相关化合物库

该产品包含在如下化合物库中:
药物功能重定位化合物库 膜蛋白靶向化合物库 抗癌上市药物库 抗癌临床化合物库 抗癌药物库 抑制剂库 GPCR靶点分子库 经典已知活性库 抗癌化合物库 FDA 上市药物库

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体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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Keywords

Naftifine hydrochloride 65473-14-5 GPCR/G Protein Microbiology/Virology Stem Cells Hedgehog/Smoothened Antibiotic Antifungal Naftifine Hydrochloride Naftifungin tinea corporis 盐酸萘替芬 pedis cruris dermatophytes inhibit Naftifine HCl Naftifine Naftin Fungal Inhibitor Exoderil inhibitor

 

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